Literature DB >> 23960753

Synthesis, characterization and anticancer activity of certain 3-{4-(5-mercapto-1,3,4-oxadiazole-2-yl)phenylimino}indolin-2-one derivatives.

Rajyalakshmi Gudipati1, Rama Narsimha Reddy Anreddy, Sarangapani Manda.   

Abstract

A series of 5- or 7-substituted 3-{4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenylimino}-indolin-2-one derivatives were synthesized by treating 5-(4-aminophenyl)-1,3,4-oxadiazole-2-thiol with different isatin derivatives. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, (1)H NMR, MS) analyses. All the synthesized derivatives were screened for anticancer activity against HeLa cancer cell lines using MTT assay. All the synthetic compounds produced a dose dependant inhibition of growth of the cells. The IC50 values of all the synthetic test compounds were found between 10.64 and 33.62 μM. The potency (IC50 values) of anticancer activity of compounds VIb-d was comparable with that of known anticancer agent, Cisplatin. Among the synthesized 2-indolinones, compounds VIb-d with halogen atom (electron withdrawing groups) at C5 position showed the most potent activity. These results indicate that C5 substituted derivatives may be useful leads for anticancer drug development in the future.

Entities:  

Keywords:  1,3,4-Oxadiazole; Anticancer activity; Indole; Isatin; MTT; Schiff bases

Year:  2011        PMID: 23960753      PMCID: PMC3744961          DOI: 10.1016/j.jsps.2011.03.002

Source DB:  PubMed          Journal:  Saudi Pharm J        ISSN: 1319-0164            Impact factor:   4.330


  22 in total

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Authors:  S K Sridhar; A Ramesh
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Authors:  S N Pandeya; D Sriram; G Nath; E De Clercq
Journal:  Pharm Acta Helv       Date:  1999-12

3.  Novel 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives: promising anticancer agents.

Authors:  Ahmed S Aboraia; Hamdy M Abdel-Rahman; Nadia M Mahfouz; Mahmoud A El-Gendy
Journal:  Bioorg Med Chem       Date:  2005-10-18       Impact factor: 3.641

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Authors:  A Monks; D Scudiero; P Skehan; R Shoemaker; K Paull; D Vistica; C Hose; J Langley; P Cronise; A Vaigro-Wolff
Journal:  J Natl Cancer Inst       Date:  1991-06-05       Impact factor: 13.506

5.  N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.

Authors:  T Ladduwahetty; R Baker; M A Cascieri; M S Chambers; K Haworth; L E Keown; D E MacIntyre; J M Metzger; S Owen; W Rycroft; S Sadowski; E M Seward; S L Shepheard; C J Swain; F D Tattersall; A P Watt; D W Williamson; R J Hargreaves
Journal:  J Med Chem       Date:  1996-07-19       Impact factor: 7.446

6.  Potent and selective nonpeptide inhibitors of caspases 3 and 7.

Authors:  D Lee; S A Long; J H Murray; J L Adams; M E Nuttall; D P Nadeau; K Kikly; J D Winkler; C M Sung; M D Ryan; M A Levy; P M Keller; W E DeWolf
Journal:  J Med Chem       Date:  2001-06-07       Impact factor: 7.446

7.  Resistance to cisplatin and adriamycin is associated with the inhibition of glutathione efflux in MCF-7-derived cells.

Authors:  Sandra Osbild; Laurent Brault; Eric Battaglia; Denyse Bagrel
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8.  Synthesis and primary cytotoxicity evaluation of 3-[[(3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-1H-2-indolinones.

Authors:  Aysel Gürsoy; Nilgün Karali
Journal:  Eur J Med Chem       Date:  2003-06       Impact factor: 6.514

9.  New colorimetric cytotoxicity assay for anticancer-drug screening.

Authors:  P Skehan; R Storeng; D Scudiero; A Monks; J McMahon; D Vistica; J T Warren; H Bokesch; S Kenney; M R Boyd
Journal:  J Natl Cancer Inst       Date:  1990-07-04       Impact factor: 13.506

10.  Anticonvulsant activity of Schiff bases of isatin derivatives.

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  4 in total

Review 1.  1,3,4-Oxadiazole Derivatives. Optical Properties in Pure and Mixed Solvents.

Authors:  Mihaela Homocianu; Anton Airinei
Journal:  J Fluoresc       Date:  2016-06-20       Impact factor: 2.217

2.  2,9-Bis(5-sulfanylidene-4,5-di-hydro-1,3,4-oxa-diazol-2-yl)-1,10-phenanthroline dimethyl sulfoxide disolvate.

Authors:  Md A Rahman; Mohammad Karim; Md Arifuzzaman; Tasneem Siddiquee; Lee M Daniels
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-02-22

Review 3.  Therapeutic potential of oxadiazole or furadiazole containing compounds.

Authors:  Ankit Siwach; Prabhakar Kumar Verma
Journal:  BMC Chem       Date:  2020-12-07

4.  Synthesis, characterization, and in vitro anticancer evaluation of novel 2,5-disubstituted 1,3,4-oxadiazole analogue.

Authors:  Avijit Mazumder; Mohammad Shaharyar
Journal:  Biomed Res Int       Date:  2014-08-10       Impact factor: 3.411

  4 in total

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